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Bioorg Med Chem Lett. 2011 May 15;21(10):2991-7. doi: 10.1016/j.bmcl.2011.03.049. Epub 2011 Mar 21.

Discovery of small molecule human FPR1 receptor antagonists.

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  • 1AstraZeneca R&D Charnwood, Bioscience, Bakewell Road, Loughborough LE11 5RH, UK.

Abstract

The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21486695
[PubMed - indexed for MEDLINE]
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